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The aim of the present research was to develop a magnetic coconut carbon composite (Fe2O3/Fe3O4@CNC) as a solid-phase extraction (SPE) sorbent for the analysis of carcinogenic N-nitrosodimethylamine (NDMA) in pharmaceuticals. Coconut composites modified with Fe2O3 and Fe3O4 were prepared and applied as SPE sorbent for the extraction of NDMA in pharmaceuticals. The sorbent was characterized with X-Ray, infrared spectroscopy and nitrogen porosimetry. The best ions for the Gas Chromatography-Mass Spectrometry with Selected Ion Monitoring (GC-MS/SIM) analysis were m/z 74 and 42 for NDMA, and m/z 80 and 46 for NDMA-d6 internal standard. System has offered great method performance in terms of sensitivity limit of quantitation (LOQ) 16 ng kg−1. The developed sorbent has enhanced the sensitivity and speed of analysis. The developed method was applied to authenticate the presence of NDMA in various pharmaceutical samples. Among the analyzed samples, NDMA impurities were relatively identified at high amounts in nizatidine samples.Highlights NDMA was verified in ranitidine, metformin and nizatidineFe2O3/Fe3O4@CNC composite was used for NDMA identification without pretreatmentSPE sorbent enhance sensitivity, reduce analysis time, sustain accuracy & precisionHigh level of NDMA impurity were found in nizatidine pharmaceuticals.

Overview of various analytical methods for estimating anti-histaminic (H2 Receptor blockers) drugs, particularly for determining their concentration percentage (assay) by analytical methods developed on analytical instruments i.e., UV visible Spectrophotometer, High-Performance Liquid Chromatography, and Hyphenated techniques. The review includes a literature survey of H2 receptor blocker drugs namely cimetidine (Tagamet), ranitidine (Zantac), famotidine (Pepcid, Pepcid AC), and nizatidine (Axid). The examined literature survey addressed chromatographic (HPLC) and UV visible spectrophotometric methods with LC-MS/MS methods used in pure forms, pharmaceutical formulations, human plasma, and other biological fluids for their estimation. In the case of validation parameters, mostly Linearity, Recovery study, LOD, and LOQ were considered and mentioned. This review helps researchers to get detailed information regarding various analytical methods of development and validation for H2 receptor antagonists. [ABSTRACT FROM AUTHOR]

Purpose: Gastrointestinal (GI) cancer occurs in digestive organs such as the stomach, colon, liver, esophagus, and pancreas. About 83,034 cases occurred in Korea alone in 2020. Dietary factors, alcohol consumption, Helicobacter pylori (H. pylori), and lifestyle factors increase the incidence of diseases such as gastritis, peptic ulcer, pancreatitis, and gastroesophageal reflux disease (GERD), which can develop into GI cancer. However, in 2019, the US Food and Drug Administration announced that the drugs ranitidine and nizatidine, which are used for digestive disorders, contain carcinogens. In this study, we investigated the effects of ranitidine and nizatidine on the development of GI cancer. Materials and methods: In this study, using National Health Insurance Service-National Sample Cohort (NHIS-NSC) version 2.5 (updated from 2002 to 2019), subjects who developed GI cancer were enrolled in the case group, and those who were at risk of, but did not develop, cancer were enrolled in the control group. Thereafter, risk-set matching was performed (1:3 ratio) by sex and age at the time of diagnosis of cancer in the case group. Through this procedure, 22,931 cases and 68,793 controls were identified. The associations of ranitidine and/or nizatidine with GI cancer were confirmed by adjusted odds ratios (aORs) and 95% confidence intervals (CIs) calculated through conditional logistic regression analysis. Results: The aORs of ranitidine and/or nizatidine users were lower than those of nonusers in all average prescription days groups (< 30 days/year: aOR [95% CI] = 0.79 [0.75-0.82]; 30-59 days/year: aOR [95% CI] = 0.66 [0.59-0.73]; 60-89 days/year: aOR [95% CI] = 0.69 [0.59-0.81]; ≥ 90 days/year: aOR [95% CI] = 0.69 [0.59-0.79]). Sensitivity analyses were conducted with different lag periods for the onset of GI cancer after drug administration, and these analyses yielded consistent results. Additional analyses were also performed by dividing subjects into groups based on cancer types and CCI scores, and these analyses produced the same results. Conclusion: Our study, using nationwide retrospective cohort data, did not find evidence suggesting that ranitidine and nizatidine increase the risk of GI cancer. In fact, we observed that the incidence of GI cancer was lower in individuals who used the drugs compared to nonusers. These findings suggest a potential beneficial effect of these drugs on cancer risk, likely attributed to their ability to improve digestive function. [ABSTRACT FROM AUTHOR]

Background/Aims Histamine-2 receptor antagonists (H2RA) are used to treat acid-related disorders and functional dyspepsia. In contrast to other H2RAs, nizatidine promotes gastric emptying (GE). We investigated the effects of nizatidine and famotidine on intragastric pH and the GE rate in rats exposed to stress. Materials and Methods We used 8-week-old male Wistar rats. Based on administration of water or drugs after an overnight fast, the animals were categorized into the nonstress-water, stress-water, stress-nizatidine, stress-famotidine, and stress-nizatidine with mosapride groups. The rats had access to pre-weighed food for 10 minutes, and those in the stress groups were exposed to 1 hour of restraint stress. Intragastric pH was measured under isoflurane anesthesia, and the GE rate was measured after the rats were sacrificed. Results The GE rate was significantly lower in the stress-water and stress-famotidine groups than in the nonstress-water group. However, GE in the stress-nizatidine and stress-nizatidine with mosapride group did not significantly differ from that in the nonstress- water group. The GE rate was significantly higher in the stress-nizatidine with mosapride than in the stress-famotidine group. Intragastric pH was significantly higher in the stress-nizatidine and stress-famotidine groups than in the stress-water group. Nonetheless, there was no significant difference in pH between the stress-nizatidine and stress-famotidine groups. The intragastric pH was slightly but significantly higher in the stress-nizatidine with mosapride group than in the stress-nizatidine and stress-famotidine groups. Conclusions In contrast to famotidine, nizatidine prevents stress-induced GE delay, which suggests that nizatidine is superior to other H2RAs for treatment of functional dyspepsia associated with delayed GE.

In this study, the degradation of nizatidine (NZTD) was investigated using a zero-valent iron-promoted divalent iron-activated persulfate process. Results show that complete NZTD degradation at 5 mg/L could be achieved under the optimal conditions of NZTD/zero-valent iron (ZVI)/Fe(II)/persulfate (PS) = 1:6:3:6 (molar ratio), pH = 7.0, and 25 °C. A highly alkaline environment would decrease the NZTD removal, and the NZTD degradation increased with the reaction temperature (5–35 °C). Furthermore, acidic conditions and the presence of Cl- enhanced the degradation of NZTD, but the presence of high doses of HCO 3 -, NO 3 -, and humic acid inhibited the degradation of NZTD. The fragile sites in NZTD were predicted by density functional theory (DFT) methods, and six transformation products were detected during the degradation of NZTD by PS/Fe(II)/ZVI. The toxicity of the intermediates was examined using the TEST toxicity prediction model and luminescent bacteria. The degradation process generated intermediates with higher toxicity than NZTD. However, after 60 min of reaction, the inhibition rate of luminescent bacteria decreased rapidly, and low toxicity products were generated. These results suggest that ZVI/Fe(II)/PS is promising as a new alternative process for the treatment of water containing NZTD. [Display omitted] • The presence of O 2 −• was detected in the ZVI/Fe(II)/PS system with 5% removal contribution. • NZTD will generate highly toxic byproducts during the degradation of ZVI / Fe(II) / PS system. • The ZVI / Fe(II) / PS system has a strong ability to resist pH changes. • Cl- can promote the degradation of NZTD in ZVI/Fe(II)/PS system. [ABSTRACT FROM AUTHOR]

Pharmaceuticals have recently emerged as a significant environmental concern due to the growth of population, expansion of industry, and the shift in modern lifestyles. Herein, we present a Fe(II)/percarbonate (SPC) process with dramatically enhanced efficiency by the introduction of zerovalent iron (ZVI). After the addition of ZVI, the removal rate of nizatidine (NZTD) went up from 71.7 to 84.2%. The removal rate of NZTD decreases with rising pH and speeds up with increasing temperature. It was found that under the condition of pH = 7 and T = 25 °C, the molar ratio of the optimal concentration of NZTD degradation in the system was [NZTD]0:[SPC]0:[Fe(II)]0:[ZVI]0 = 1:8:24:16, with a degradation rate of 99.8%. At the same time, target pollutants can also be successfully eliminated from actual water bodies. Moreover, we test for toxicity using luminescent bacteria, and the results demonstrate that the system is capable of effectively decreasing the toxicity of NZTD. The research findings can contribute to the clarification of the migration and transformation law of NZTD in the oxidation process, thereby providing a scientific basis and technical support for the removal of NZTD in the tertiary water treatment for a water source. [ABSTRACT FROM AUTHOR]

Pharmaceuticals, especially amine-based pharmaceuticals, such as nizatidine and ranitidine, contaminate water and resist water treatment. Here, different amounts of graphene sheets are coupled with g-C3N4 nanosheets (wt% ratio of 0.5, 1, 3 and 5 wt% of graphene) to verify the effect of surface plasmon resonance introduced to the g-C3N4 material. The synthesized materials were systematically examined by advanced analytical techniques. The prepared photocatalysts were used for the degradation of amine-based pharmaceuticals (nizatidine and ranitidine). The results show that by introducing only 3 wt% graphene to g-C3N4, the absorption ability in the visible and near-infrared regions dramatically enhanced. The absorption in the visible range was 50 times higher when compared to the pure sample. These absorption features suggest that the surfaces of the carbon nitride sheet are covered by the graphene nanosheet, which would effectively apply the LSPR properties for catalytic determinations. The enhancement in visible light absorption in the composite was confirmed by PL analysis, which showed greater inhibition of the electron-hole recombination process. The XRD showed a decrease in the (002) plan due to the presence of graphene, which prevents further stacking of carbon nitride layers. Accordingly, the Gr/g-C3N4 composite samples exhibited an enhancement in the photocatalytic performance, specifically for the 5% Gr/g-C3N4 sample, and close to 85% degradation was achieved within 20 min under solar irradiation. Therefore, applying the Gr/g-C3N4 for the degradation of a pharmaceutical can be taken into consideration as an alternative method for the removal of such pollutants during the water treatment process. This enhancement can be attributed to surface plasmon resonance-induced photocatalysis in a 2D/2D graphene/g-C3N4 heterostructure. [ABSTRACT FROM AUTHOR]

The aim of the present research was to develop a magnetic coconut carbon composite (Fe2O3/Fe3O4@CNC) as a solid-phase extraction (SPE) sorbent for the analysis of carcinogenic N-nitrosodimethylamine (NDMA) in pharmaceuticals. Coconut composites modified with Fe2O3 and Fe3O4 were prepared and applied as SPE sorbent for the extraction of NDMA in pharmaceuticals. The sorbent was characterized with X-Ray, infrared spectroscopy and nitrogen porosimetry. The best ions for the Gas Chromatography-Mass Spectrometry with Selected Ion Monitoring (GC-MS/SIM) analysis were m/z 74 and 42 for NDMA, and m/z 80 and 46 for NDMA-d6 internal standard. System has offered great method performance in terms of sensitivity limit of quantitation (LOQ) 16 ng kg−1. The developed sorbent has enhanced the sensitivity and speed of analysis. The developed method was applied to authenticate the presence of NDMA in various pharmaceutical samples. Among the analyzed samples, NDMA impurities were relatively identified at high amounts in nizatidine samples. NDMA was verified in ranitidine, metformin and nizatidine Fe2O3/Fe3O4@CNC composite was used for NDMA identification without pretreatment SPE sorbent enhance sensitivity, reduce analysis time, sustain accuracy & precision High level of NDMA impurity were found in nizatidine pharmaceuticals. [ABSTRACT FROM AUTHOR]

Background: For the treatment of gastritis, rebamipide, a mucoprotective agent, and nizatidine, a gastric acid suppressant, are commonly employed individually., Aim: To compare the efficacy of Mucotra ® SR (rebamipide 150 mg) and Axid ® (nizatidine 150 mg) combination therapy with the sole administration of Axid ® in managing erosive gastritis., Methods: A total of 260 patients diagnosed with endoscopically confirmed erosive gastritis were enrolled in this open-label, multicenter, randomized, phase 4 clinical trial, allocating them into two groups: Rebamipide/nizatidine combination twice daily vs nizatidine twice daily for 2 weeks. The full-analysis set analysis encompassed 239 patients (rebamipide/nizatidine, n = 121; nizatidine, n = 118), while the per-protocol analysis included 218 patients ( n = 110 vs 108). Post-treatment assessments comprised primary (erosion improvement rate) and secondary (erosion and edema cure rates, erythema improvement rates, hemorrhage, and gastrointestinal symptoms) endpoints. Furthermore, drug-related adverse effects were evaluated., Results: Primary efficacy assessment showed a statistically significant improvement rate in mucosal erosions in the combination group compared to the control group in the full-analysis set (rebamipide/nizatidine 62.0%, nizatidine 49.2%, P = 0.046), with a similar trend noted in the per-protocol analysis (62.7% vs 50.0%, P = 0.058). Both groups were effective in curing erosion and edema and improvement of bleeding, erythema, and gastrointestinal symptoms, whereas no inter-group differences were noted. When confined to the participants with gastritis symptoms, improvement of erosion was more optimal in the combination group (63.0% vs 49.5%, P = 0.046). No adverse events related to the drugs were observed., Conclusion: Rebamipide/nizatidine combination is effective in treatment of erosive gastritis., Competing Interests: Conflict-of-interest statement: All the authors report no relevant conflicts of interest for this article., (©The Author(s) 2024. Published by Baishideng Publishing Group Inc. All rights reserved.)

Abstract Nizatidine is an anti-secretogogue and a gastroprotective drug with a half-life of 1-2 h and is well absorbed in the stomach. This study aimed to optimize the process and develop floating microparticles of nizatidine that are based on low methoxyl pectin. Oil-in-oil dispersion method and Taguchi orthogonal array design were employed, and the prolonged residence time of the microparticles in the stomach was demonstrated. The constraints for independent variables, viz. A-polymer, B-internal solvent volume, C-surfactant, D-stirring rate and E-stirring time were set to generate the experimental runs. Particle size, percentage yield, micromeritic properties, entrapment efficiency, in vitro buoyancy and in vitro release were characterized. Surface morphology, zeta potential, in vitro release kinetics and in vivo floating performance of the optimized formulation was examined. The microparticles were free-flowing, irregular in shape and had a mean particle size distribution of 73-187 μ. Low methoxyl pectin played a predominant role in achieving buoyancy and optimum gastric retention for the modified release of the drug, suggesting Korsmeyer-Peppas model as the possible release mechanism. In vivo radiographic study in rabbits revealed that the drug was retained in the stomach for a period of 6 h. These results indicate that nizatidine floating microparticulate system provides modified drug release for the effective treatment of gastric ulcer.

Background and objectivesIn the proximal tubule, basic drugs are transported from the renal cells to the tubule lumen through the concerted action of the H(+)/organic cation antiporters, multidrug and toxin extrusion (MATE) 1 and MATE2K. Dual inhibitors of the MATE transporters have been shown to have a clinically relevant effect on the pharmacokinetics of concomitantly administered basic drugs. However, the clinical impact of selective renal organic cation transport inhibition on the pharmacokinetics and pharmacodynamics of basic drugs, such as metformin, is unknown. This study sought to identify a selective MATE2K inhibitor in vitro and to determine its clinical impact on the pharmacokinetics and pharmacodynamics of metformin in healthy subjects.MethodsStrategic cell-based screening of 71 US Food and Drug Administration (FDA)-approved medications was conducted to identify selective inhibitors of renal organic cation transporters that are capable of inhibiting at clinically relevant concentrations. From this screen, nizatidine was identified and predicted to be a clinically potent and selective inhibitor of MATE2K-mediated transport. The effect of nizatidine on the pharmacokinetics and pharmacodynamics of metformin was evaluated in 12 healthy volunteers in an open-label, randomized, two-phase crossover drug-drug interaction (DDI) study.ResultsIn healthy volunteers, the MATE2K-selective inhibitor nizatidine significantly increased the apparent volume of distribution, half-life, and hypoglycemic activity of metformin. However, despite achieving unbound maximum concentrations greater than the in vitro inhibition potency (concentration of drug producing 50% inhibition [IC50]) of MATE2K-mediated transport, nizatidine did not affect the renal clearance (CLR) or net secretory clearance of metformin.ConclusionThis study demonstrates that a selective inhibition of MATE2K by nizatidine affected the apparent volume of distribution, tissue concentrations, and peripheral effects of metformin. However, nizatidine did not alter systemic concentrations or the CLR of metformin, suggesting that specific MATE2K inhibition may not be sufficient to cause renal DDIs with metformin.

Abstract Background The present research was aimed in developing gastroretentive tablets of Nizatidine, in order to increase the bioavailability of the drug. Nizatidine belongs to BCS class 3 and thus formulating into gastroretentive tablets helps to achieve a better therapeutic effect. There were no reports available on the use of Mimosa gum in the design of gastroretentive drug delivery systems. Response surface methodology was employed to optimize the formulation with suitable experimental design. The goal of the response surface methodology was to obtain a regression model and to find a suitable approximation for the true functional relationship between the response and the set of independent variables. Hence, the statistical approach like full factorial design was utilized to obtain optimized formulation with a smaller number of experiments. Results DSC study justified no interaction of the drug with excipients. The floating lag time was observed to be less than 20 s, total floating time was in the range of 8–24 h, hardness ranges from 4 to 5 kg/cm2, and friability was less than 1%. Dissolution data indicated that the higher viscosity of Mimosa (2%) delayed the drug release for extended period of time up to 23 h when compared to lower viscosity Mimosa (1%), which controlled the release of the drug up to 12 h only. The ‘n’ values of all the prepared formulations were found to be 0.59 to 0.81 indicating that the release mechanism followed anomalous (non-Fickian) diffusion. The optimal values of independent test variables were obtained from the overlay plots. The optimized formulation of Mimosa gum (2%) (M2%opt) contained 170 mg of polymer and 25.5 mg (15%) of sodium bicarbonate. Similarly, the optimized formulation of Mimosa (1%) (M1%opt) contained 255 mg of polymer and 34 mg (10%) of sodium bicarbonate. Conclusion The results clearly indicated that the optimized formulations followed zero-order release kinetics with diffusion mechanism as per the predicted theoretical release rate confirming the suitability of the predicted theoretical release profile.

Nizatidine (NIZ), a histamine H2-receptor antagonist, is soluble and stable in the stomach, however, it exhibits a short half-life and a rapid clearance. Therefore, chitosan (CS) and polyethylene oxide (PEO) nanofibers (NFs) at different weight ratios were prepared by electrospinning and characterized. The selected uncrosslinked and glutaraldehyde-crosslinked NFs were investigated regarding floating, solid-state characteristics, in vitro release, and in vitro cytotoxicity. The cytoprotective activity against ethanol-induced gastric injury in rats was evaluated through macroscopical, histopathological, immunohistochemical, and oxidative stress examinations. NFs based on 8:2 CS:PEO exhibited the smallest diameter (119.17 ± 22.05 nm) and the greatest mucoadhesion (22.82 ± 3.21 g/cm2), so they were crosslinked with glutaraldehyde. Solid-state characterization indicated polymers interaction, a successful crosslinking, and NIZ dispersion in NFs. Crosslinking maintained swollen mats at pH 1.2 (swelling% = 29.47 ± 3.50% at 24 h), retarded their erosion at pH 6.8 (swelling%= 84.64 ± 4.91% vs. 25.40 ± 0.79% for the uncrosslinked NFs at 24 h), augmented the floating up to 24 h vs. 10 min for the uncrosslinked NFs at pH 1.2 and prolonged the drug release (%drug released ≥ 93% at 24 h vs. 4 and 5 h for the uncrosslinked NFs at pHs 1.2 and 6.8, respectively). The viability of Caco-2 cells ≥ 86.87 ± 6.86% revealed NFs biocompatibility and unreacted glutaraldehyde removal. Crosslinking of 8:2 CS:PEO NFs potentiated the antiulcer activity (38.98 vs. 8.67 for the uncrosslinked NFs) as well as it preserved the gastric wall architecture, COX-2 expression, and oxidative stress markers levels of the normal rats.

Abstract Background Peptic ulcer is an excoriated area of stomach or intestinal mucosa. Two experimental designs were proceeded: the first aimed. on twenty adult male albino rats, used to study the protective effect of both ranitidine and nizatidine; on the second, including sixty adult male albino rats, was used to study the therapeutic effect of ranitidine and nizatidine after induction of ulcer and also to evaluate the adverse effects of therapeutic doses of H2-receptor antagonists on male hormonal profile. The study aims to assess the gastroprotective effects of nizatidine and ranitidine and on treating of non-steroidal anti-inflammatory drugs (NSAIDs) induced peptic ulcer and to evaluate its adverse effect on male sex hormones. Result The result revealed that ranitidine and nizatidine reduced incidence of ulceration. Histopathological findings showed a significant recovery of the alteration, and disturbance in male sex hormones. Conclusion Nizatidine is better than ranitidine in the management of NSAIDs induced peptic ulcer in rats.

Expired nizatidine drug (END) was studied as inhibitor for a-brass in 1M HCl utilizing weight loss (WL), and electrochemical methods namely, AC impedance (EIS), Potentiodynamic polarization (PP), and electrochemical frequency modulation (EFM) tests. The protection efficiency (%IE) was improved with raising in the dose of the expired nizatidine and decreases with raising the temperature. The (%IE) reaching maximum value 95 % at higher dose of expired nizatidine drug at 25°C. PP data indicated that nizatidine drug behaves like a mixed kind drug. The protection of a-brass corrosion by nizatidine can fit to the adsorption ability of nizatidine drug molecules onto the reactive sites of the a-brass surface. The adsorption of the drug follows Langmuir adsorption isotherm. The surface morphology of a-brass was investigated. The results obtained from different methods are in excellent agreement.

Nizatidine (NIZ), a histamine H2-receptor antagonist, is soluble and stable in the stomach, however, it exhibits a short half-life and a rapid clearance. Therefore, chitosan (CS) and polyethylene oxide (PEO) nanofibers (NFs) at different weight ratios were prepared by electrospinning and characterized. The selected uncrosslinked and glutaraldehyde-crosslinked NFs were investigated regarding floating, solidstate characteristics, in vitro release, and in vitro cytotoxicity. The cytoprotective activity against ethanol-induced gastric injury in rats was evaluated through macroscopical, histopathological, immunohistochemical, and oxidative stress examinations. NFs based on 8:2 CS:PEO exhibited the smallest diameter (119.17 ± 22.05 nm) and the greatest mucoadhesion (22.82 ± 3.21 g/cm2), so they were crosslinked with glutaraldehyde. Solid-state characterization indicated polymers interaction, a successful crosslinking, and NIZ dispersion in NFs. Crosslinking maintained swollen mats at pH 1.2 (swelling% = 29.47 ± 3.50% at 24 h), retarded their erosion at pH 6.8 (swelling%= 84.64 ± 4.91% vs. 25.40 ± 0.79% for the uncrosslinked NFs at 24 h), augmented the floating up to 24 h vs. 10 min for the uncrosslinked NFs at pH 1.2 and prolonged the drug release (%drug released = 93% at 24 h vs. 4 and 5 h for the uncrosslinked NFs at pHs 1.2 and 6.8, respectively). The viability of Caco-2 cells = 86.87 ± 6.86% revealed NFs biocompatibility and unreacted glutaraldehyde removal. Crosslinking of 8:2 CS:PEO NFs potentiated the antiulcer activity (38.98 vs. 8.67 for the uncrosslinked NFs) as well as it preserved the gastric wall architecture, COX-2 expression, and oxidative stress markers levels of the normal rats. [ABSTRACT FROM AUTHOR]

INTRODUCTION: The first intervention needed for ischaemic tissue is to restore blood flow. However, the abundant molecular oxygen that is supplied to the ischaemic tissue via arterial blood after reperfusion results in the formation of excessive free oxygen radicals and oxidative stress. This suggests a potential benefit from treatment with antioxidants for reducing the ischaemia-reperfusion (I/R) damage. In our study, we investigated the effect of nizatidine, an H2 receptor antagonist antiulcer drug for the treatment of peptic ulcers, on renal I/R damage. The cytoprotective effect of nizatidine is known to originate from its antioxidant characteristics. No information was found in the literature regarding the protective effect of nizatidine on renal I/R damage. The objective of this study was to investigate the effect of nizatidine on oxidative renal damage induced in rats by I/R. METHODS: In this study, albino Wistar male rats were grouped into renal ischaemia-reperfusion (RIR), nizatidine 50 mg/kg + renal ischaemia-reperfusion (NIR-50), and sham surgery (SG) conditions. RESULTS: Our biochemical test results showed that oxidative stress markers, such as malondialdehyde (MDA) and myeloperoxidase (MPO), increased significantly (p

Gastroretentive drug delivery is one of the targeted strategy for prolonging gastric residence time, in management of peptic ulcer along with optimizing site-specific drug release for local or systemic impact in the upper gastrointestinal tract (GIT). Many gastroretentive drug delivery methods have been designed and developed over the last few decades. In present research, we have developed oral sustained release in-situ floating gel as a carrier for stomach specific delivery of anti Nizatidine (NZD). NZD is an antagonist of histamine H2-receptor. It is used commonly in severe duodenal ulcers, stomach ulcers, ulcerative esophagitis, heartburn. Nevertheless, the recent failure of proton pump inhibitors to suppress nighttime gastric acid spike (related to high nocturnal histamine concentration) and side effects from other H2-receptor antagonists (gyanacomastia) open a new path to NZD delivery at specific times in relation to symptom onset. Around 10 batches (F1-F10) were formulated and were subjected to determination of f2 value, viscosity (cps), gel strength (dyne/cm2), pH, drug content and in-vivo pharmacokinetic study. In-vivo investigations demonstrated that there was a marked difference in the reduction of ulcer index and volume of gastric acid secretion from nizatidine in situ gelling formulation (for optimized batch F6) when compared with the plain nizatidine solution (P < 0.01) and control group (P < 0.001). So, an effective oral sustained release in-situ floating gel as a carrier for stomach specific delivery of anti Nizatidine were formulated and evaluated successfully. [ABSTRACT FROM AUTHOR]

Gastroretentive drug delivery is one of the main methods for prolonging gastric occupancy, peptic ulcer control and site-specific medication release enhancement for local or systemic effects in the upper gastrointestinal tract (GIT). Several approaches for the distribution of gastroretentive drugs have been planned and developed over the last few decades. We also developed oral sustained release in-situ floating gel as a carrier for the transmission of anti-nizatidine (NZD) unique to the stomach in present work. NZD is histamine H2-receptor antagonist. This is usually seen in extreme duodenal ulcers, stomach ulcers, heartburn, ulcerative esophagitis. Nonetheless, the recent inability of proton pump inhibitors to counteract the increase in gastric acid at night (related to elevated production in histamine at night) and side effects from certain H2 receptor antagonists (gyanacomastia) open up a different route to NZD transmission at particular periods in relation to the initiation of symptoms. Approximately 10 lots (F1-F10) were formulated and subjected to determination of f2 performance, viscosity (cps), gel strength (dyne / cm2), pH, product quality, and pharmacokinetic in vivo research. In-vivo experiments revealed a significant difference in the reduction of the ulcer index and the amount of gastric acid secretion from the formulation of nizatidine in situ gelling (for optimized batch F6) relative to the nizatidine solution (P < 0.01) and control group (P < 0.001). As a result, an efficient oral sustained release in-situ floating gel was developed and tested effectively as a carrier for stomach-specific distribution of anti Nizatidine. [ABSTRACT FROM AUTHOR]

[Display omitted] • Cantaloupe seeds and mush have been used as a substrate for synthesis of N-CQDs for the first time. • Ultrafast green microwave-driven synthesis of self-doped N-CQDs has been developed. • The synthesis process is superior to other reported synthesis methods. • The green N-CQDs have high stability, water solubility, and intense blue fluorescence. • The N-CQDs have been applied as a sensitive fluorescence sensor for Nizatidine in urine and capsules. In the current study, a fast, ecological, one-pot, and cost-efficient method was developed for the synthesis of nitrogen-doped carbon quantum dots (N-CQDs) using plant wastes. This method includes the treatment of cantaloupe seeds and mush by microwave for four-minutes as a re-cyclable, green, and cheap carbon and nitrogen source. The furnished N-CQDs show a fluorescence quantum yield of 13.15 %, excellent water solubility, and high stability. A full characterization of the plant waste-derived quantum dots revealed the self-doping with nitrogen. The synthesized N-CQDs have been applied as an efficient nanoprobe for fluorometric determination of nizatidine (NZT), a gastroprotective drug, at λ ex /λ em of 325/416 nm within the concentration range of 0.75–100.0 μM and LOD of 0.24 μM. The N-CQDs show excellent selectivity for NZT in the presence of various possibly co-existing substances. Excellent mean % recovery was achieved for the determination of NZT in capsules (101.97 ± 0.91 %). Moreover, the N-CQDs were used for the determination of NZT in human urine within the concentration range of 2.5–100.0 μM with LOD of 0.8 μM, therefore it has been applied for monitoring the excretion profile of NZT in urine. The greenness of the proposed probe has been evaluated using two greenness software and metrics proving excellent greenness feature that is attributed to using a renewable and cheap plant waste product as a feedstock via low-energy/low-cost microwave-assisted synthesis, elimination of organic solvents and hazardous chemicals, and relying on a direct mix-and-read assay. [ABSTRACT FROM AUTHOR]

Nizatidine is a histamine H2 receptor antagonist. This compound belongs to the class of organic compounds known as 2,4‐di‐substituted thiazoles. These are the compounds containing a thiazole ring. It inhibits the action of histamine mediated by H2 receptors such as gastric acid and pepsin output and the drug is used for the treatment of duodenal ulcers. This review presents an overview about the different analytical methods for the analysis of Nizatidine and its metabolite in biological fluids, commercial products, and simultaneous estimation of other H2 receptor antagonist in commercial products. The most commonly used analytical method for Nizatidine is high‐performance liquid chromatography. This review also gives information about pharmacokinetics, its application and susceptibility of H2 receptor antagonist to metabolism by gastrointestinal flora. [ABSTRACT FROM AUTHOR]

Nizatidine is a gastroprotective drug with a short biological half-life and narrow absorption window. This study aimed at developing floating tablets of nizatidine using various HPMC viscosity grades, namely K4M, E4M, K15 and K200M. Directly compressed tablets revealed an excellent uniformity in hardness, thickness and weight and nizatidine was evenly distributed within the matrix floating tablets. Buoyancy study revealed floating lag time as low as 18–38 s, and tablets remain buoyant for upto 24 h. However, the later depended upon viscosity grade of HPMC and that the higher the viscosity, the less was the total floating time. In vitro dissolution indicated viscosity dependent nizatidine release from the floating tablets. HPMC K4M and E4M based floating tablets released almost 100% drug in 12 h, whilst higher viscosity polymers such as K15 and K200M only released 81.88% and 75.81% drug, respectively. The drug release followed non-Fickian diffusion from tablets formulated with K4M, K15 and K200M, whilst super case II transport was observed with E4M based tablets. More interestingly, K4M and E4M polymers have similar viscosity yet exhibited different drug release mechanism. This was attributed to the difference in degree of substitution of methoxyl- and hydroxypropoxyl- groups on polymer backbone.

Background Gastric accommodation is a reflex reaction related to gastric reservoir function. Psychological stress, such as anxiety, inhibits gastric accommodation in humans. Acotiamide enhances the effect of acetylcholine in the enteric nervous system, enhances gastric contractility, and accelerates delayed gastric emptying. However, the effect of acotiamide on stress-induced impaired gastric accommodation remains unclear. Therefore, we examined the effect of acotiamide on gastric accommodation and stress-induced impaired gastric accommodation using a conscious guinea pig model. Methods A polyethylene bag was inserted through the distal region of the gastric body into the proximal stomach of 5-week-old male Hartley guinea pigs. Gastric accommodation was evaluated by measuring the intrabag pressure in the proximal stomach after oral administration of a liquid meal. In the stress model, animals were subjected to water-avoidance stress. Acotiamide (Z-338) or nizatidine was administered subcutaneously. Fecal output was determined as the number of fecal pellets. Key Results Administration of the liquid meal significantly decreased intrabag pressure, indicating induction of gastric accommodation. Acotiamide treatment prolonged liquid meal-induced gastric accommodation and significantly increased the number of fecal pellets compared to controls. Water-avoidance stress significantly inhibited liquid meal-induced gastric accommodation. Pretreatment with acotiamide significantly improved stress-induced impaired gastric accommodation. The number of fecal pellets in the acotiamide group increased significantly compared to controls. Acotiamide, but not nizatidine, significantly decreased gastric emptying. Conclusions & Inferences Acotiamide prolongs gastric accommodation and improves stress-induced impaired gastric accommodation, indicating a potential role for acotiamide in the treatment of functional dyspepsia through its effects on gastric accommodation reactions. [ABSTRACT FROM AUTHOR]

The dielectric properties of two pharmaceuticals nizatidine and perphenazine were investigated in the supercooled liquid and glassy states by broadband dielectric spectroscopy. Two relaxation processes were observed in both the pharmaceuticals. The relaxation process observed above the glass transition temperature is the structural alpha relaxation and below the glass transition temperature is the gamma relaxation of intramolecular origin. The Johari-Goldstein beta relaxation coming from the motion of the entire molecule is found to be hidden under the structural relaxation peak in both the pharmaceuticals. [ABSTRACT FROM AUTHOR]

[Display omitted] • The MOF on MOF composite P21-3 was synthesized using an epitaxial growth strategy. • The light absorption capacity and specific surface area of P21-3 were enhanced. • Photodegradation efficiency of P21-3 for nizatidine reached 90.81% in 120 min. • The dimethylamine functional group in nizatidine had been destroyed. • N-nitrosodimethylamine was not produced in the photodegradation process. MOF on MOF composites illustrated superb functional scalability, but few MOF on MOF composites had been applied in the direction of photocatalytic degradation. In this work, a series of P21-X (X = 1, 2, 3, 4) composites were synthesized and optimized with PCN-134 as the MOF seed and PCN-222 as the secondary MOF by an epitaxial growth method and applied to the photocatalytic degradation of nizatidine (NZT). P21-X had excellent substantial adsorption and photocatalytic properties. P21-3 exhibited the highest removal of 90.81% for NZT. The mechanism of P21-3 producing 1O 2 was probed. Based on the results of UPLC-HRMS, the NDMA was not produced during the degradation process and rational pathways for degradation of NZT were proposed. The environmental toxicity of NZT degradation products was evaluated using ECOSAR, T.E.S.T. software and Vibrio fischeri luminescence inhibition, the results showed that the toxicity of the reaction solution was diminished after 120 min of photodegradation by P21-3. Moreover, given the strong anti-interference performance of 1O 2 , the photocatalytic degradation system constructed with P21-3 could be free from the interference of common anions, cations and dissolved organic matters. As a result, the photocatalytic activity of the system remained high removal of NZT in tap water, river water and seawater. The results demonstrated that the MOF on MOF composites P21-3, synthesized by the epitaxial growth method, had enhanced photodegradation capability. The current study not only avoids the generation of toxic by-products in the photocatalytic degradation process but also broadens the application area of MOF on MOF composites. [ABSTRACT FROM AUTHOR]

This work describes the stability-indicating determination of the H2-receptor antagonist nizatidine in its bulk and capsules dosage form using high performance liquid chromatography coupled with diode array detector (HPLC-DAD). The developed method involved the use of Thermo Hypersil BDS-C8 (4.6 × 250 mm, 5 μm particle size) column and a mobile phase composed of 0.05 M phosphoric acid and acetonitrile (50:50, v/v). The mobile phase was pumped at a flow rate of 1 mL/min. Quantification of nizatidine was based on measuring its peak area at 320 nm. The retention time for nizatidine was about 3.61 min. The reliability and analytical performance of the proposed HPLC procedure were statistically validated with respect to linearity, range, precision, accuracy, specificity, robustness, detection and quantification limits. Calibration curve of nizatidine was linear in the range of 5–50 μg/mL with correlation coefficient >0.9999. The drug was subjected to forced-degradation conditions of acidic and basic hydrolysis, oxidation, dry heat and UV photolysis where it showed considerable degradation in basic and oxidative conditions. The proposed method proved to be specific and stability-indicating by resolution of the drug from its forced-degradation products. The validated HPLC method was applied to the analysis of nizatidine in capsules dosage form where it was quantified with recoveries not less than 98.2%. Assay results were statistically compared to USP 2011 pharmacopeial method where no significant difference was observed between the proposed and reference methods.